Adipotide Powder is a synthetic peptide lyophilized powder for research use only. Chemically, it is a 33-amino acid polypeptide composed of a homing sequence (CKGGRAKDC) and a pro-apoptotic sequence ((KLAKLAK)₂) linked by a linker. This product is primarily used as an experimental tool compound for basic research on obesity, type 2 diabetes, and related metabolic diseases. Its mechanism of action involves targeting the prohibitin/Annexin A2 receptor complex on the surface of vascular endothelial cells in white adipose tissue, inducing endothelial cell apoptosis, cutting off blood supply to fat cells, and thus causing ischemic death of adipocytes. Animal experimental data show that subcutaneous injection (0.43 mg/kg) over 28 days in obese rhesus monkeys resulted in an average weight reduction of 11% and a reduction in total fat mass of 38-39%.
Basic Product Information
| Item | Details |
|---|---|
| Product Name | Adipotide / FTPP (Fat-Targeted Proapoptotic Peptide) / HKPao |
| CAS Number | 859216-15-2 |
| Molecular Formula | C₁₁₁H₂₀₆N₃₆O₂₈S₂ |
| Molecular Weight | Approx. 2557.2 g/mol (varies slightly with different salt forms; acetate form approx. 2617.23) |
| Appearance | White lyophilized (freeze-dried) powder |
| Purity | Typically claimed to be above 95%-99% |
| Amino Acid Sequence | CKGGRAKDC-GG-D(KLAKLAK)₂ |
| Storage Conditions | Powder: -20°C frozen, protect from light, moisture-proof; After reconstitution: short-term storage at 2°C-8°C, or long-term storage at -80°C |
| Packaging Specifications | Commonly available as 2mg/vial, 5mg/vial, 10mg/vial, or priced per gram |
Main research uses
1. Treatment of Obesity
Adipotide Powder achieves weight loss through a unique mechanism, rather than suppressing appetite or preventing fat absorption like traditional weight-loss drugs:
- Target: Directly acts on the blood supply system of white adipose tissue (the main type of fat stored in the body)
- How it works: The growth and survival of fat cells depend on the delivery of oxygen and nutrients by the surrounding capillaries. Adipotide can identify and attack the blood vessels that nourish fat, causing damage to the vascular structure.
- End result: With blood supply cut off, fat cells gradually die due to ischemia and are subsequently metabolized by the body's own clearance mechanisms.
- Animal data: In studies of obese rhesus monkeys, after 28 days of treatment, average weight decreased by about 11%, and total body fat decreased by about 38-39%.
2. Improved Metabolic Health
The value of Adipotide is not only reflected in changes in weight, but its effects on metabolic indicators are even more rapid:
- Speed of action: Within only 2-3 days of starting treatment, several metabolic indicators show significant improvement, earlier than significant weight loss.
- Insulin sensitivity: Improved, meaning the body can use blood sugar more efficiently, reducing the burden on the pancreas.
- Glucose tolerance: Improved, indicating that blood sugar fluctuations after eating become more stable and less prone to large spikes and drops.
- Blood lipid levels: Blood triglycerides show a decrease. Trends suggest a potential reduction in cardiovascular risk.
- Possible Mechanism: This compound may directly affect the endocrine function of adipose tissue, such as reducing the release of inflammatory factors.
3. Supporting Cancer Research
Adipotide entered Phase I human clinical trials, but its application scenario differs from ordinary weight loss:
- Study Subjects: Not the general obese population, but patients with castration-resistant prostate cancer (these patients have developed resistance to standard hormone therapy).
- Scientific Basis: Adipose tissue is not a passive energy storage depot; it secretes various bioactive substances, some of which may promote tumor growth and spread.
- Research Hypothesis: Significantly reducing the total body fat of patients may lower the levels of these cancer-promoting factors, thereby delaying cancer progression to some extent.
- Trial Positioning: Adipotide was used as an adjunct in this trial, with the primary goal of observing whether fat loss could have a positive impact on tumor progression, rather than as a direct anti-cancer drug.
Mechanism of Action
Adipotide is a synthetic peptide that works through apoptosis (programmed cell death). It has a unique bipartite structure:
- "Homing" sequence: This part seeks out and specifically binds to surface proteins (such as prohibitin) that supply white fat cells.
- "Killing" sequence: Once attached, this part is taken up by the cell and damages the mitochondria, thereby triggering apoptosis and cutting off the blood supply to fat.
Complete Mechanism of Action:
- After intravenous or subcutaneous injection, adipotide is distributed throughout the body via the bloodstream.
- Its homing sequence binds to the prohibitin/Annexin A2 receptor on the surface of white adipose tissue vascular endothelial cells.
- The pro-apoptotic sequence is endocytosed into the endothelial cells, disrupting mitochondria and inducing endothelial cell apoptosis.
- Following endothelial cell death, the capillary network supplying the specific adipose region collapses, leading to local ischemia.
- Adipocytes undergo secondary death due to hypoxia and nutrient deficiency (via necrosis or apoptosis).
- Dead adipocytes and endothelial cell debris are cleared by macrophages.
The white adipose tissue in this area is replaced by fibrous tissue, resulting in a permanent reduction in the number of adipocytes.
Adipotide powder is an experimental drug candidate that treats obesity and related metabolic diseases by "cutting off the blood supply to fat cells and inducing apoptosis in adipocytes." Its unique irreversible fat clearance mechanism contrasts sharply with existing drugs (such as GLP-1 receptor agonists), but it also comes with safety challenges such as nephrotoxicity.
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